Pyridine → HCID 67336322, compound

Participants

Reaction Conditions

Reaction Steps

320 mg of 2-amino-N-{4-[3-chloro-4-(3-fluoro-benzyloxy)-phenylamino]-7-(2-methoxyethoxy)-quinazolin-6-yl}-acetamide as a starting material was dissolved in 10 ml of THF, and cooled to 0° C. The solution was reacted with 0.06 ml of acrylic acid, 0.1 ml of pyridine and 234 mg of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride at 0° C. for 1 hour and at room temperature for 5 hours. The reacted solution was extracted with a mixture of chloroform and isopropanol after adding saturated sodium bicarbonate, dried over anhydrous sodium sulfate, filtered and distilled under a reduced pressure, and the resulting residue was subjected to column chromatography (eluent-ethylacetate:methanol=30:1) to obtain the title compound (96 mg, 27%).

Provenance & Evidence